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PHARMACO PRELIMS > Autonomic Pharmacology (book) > Flashcards

Autonomic Pharmacology (book) Flashcards

1
Q

the nervous system can be divided into two major subdi- visions:

A

autonomic and somatic

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2
Q

is largely independent in that its activities are not under direct conscious control

A

autonomic nervous system

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3
Q

concerned primarily with control and integration of visceral functions necessary for life such as cardiac output, blood flow distribution, and digestion.

A

autonomic nervous system

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4
Q

largely concerned with consciously controlled functions such as movement, respiration, and posture.

A

somatic

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5
Q

Chemical transmission takes place through the release of small amounts of ____ from the nerve terminals into the synaptic cleft.

A

transmitter substances

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6
Q

The ANS lends itself to division on anatomic grounds into two major portions:

A

the sympathetic (thoracolumbar) division and the parasympathetic (traditionally “craniosacral,”

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7
Q

The sympathetic preganglionic fibers leave the CNS through the

A

thoracic, lumbar, and sacral spinal nerves

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8
Q

The parasympathetic preganglionic fibers leave the CNS through the

A

cranial nerves
*especially the third, seventh, ninth, and tenth

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9
Q

Most thoracic and lumbar sympathetic preganglionic fibers are short and terminate in ganglia located in the __ chains that lie on either side of the spinal column.

A

paravertebral

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10
Q

Most of the remaining sympathetic preganglionic fibers are somewhat longer and termi- nate in ___, which lie in front of the vertebrae, usually on the ventral surface of the aorta.

A

prevertebral ganglia

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11
Q

Some preganglionic parasympathetic fibers terminate in parasympathetic ganglia located outside the organs innervates:

A

the ciliary, pterygopalatine, submandibular, and otic ganglia.

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12
Q

Several pelvic ganglia are innervated by ___ that are ontogenetically similar to sympathetic preganglionic fibers

A

sacral preganglionic nerves

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13
Q

A large and highly orga- nized collection of neurons located in the walls of the gastrointes- tinal (GI) system

A

enteric nervous system (ENS)

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14
Q

The ENS includes the

A

myenteric plexus (the plexus of Auerbach) and the submucous plexus (the plexus of Meissner)

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15
Q

The primary transmitter at ANS ganglia, at the somatic neuromuscular junction, and at parasympathetic postganglionic nerve endings.

A

Acetylcholine (ACh)

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16
Q

A primary excitatory transmitter to smooth muscle and secretory cells in the ENS. Probably also the major neuron-to-neuron (“ganglionic”) transmitter in the ENS.

A

Acetylcholine

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17
Q

Acts as a transmitter or cotransmitter at many ANS-effector synapses

A

Adenosine triphosphate (ATP)

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18
Q

Found with substance P in cardiovascular sensory nerve fibers. Present in some secretomotor ENS neurons and interneurons. A cardiac stimulant

A

Calcitonin gene-related peptide (CGRP)

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19
Q

May act as a cotransmitter in some excitatory neuromuscular ENS neurons

A

Cholecystokinin (CCK)

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20
Q

A modulatory transmitter in some ganglia and the ENS. Possibly a postganglionic sympathetic transmitter in renal blood vessels

A

Dopamine

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21
Q

Present in some secretomotor and interneurons in the ENS. Appear to inhibit ACh release and thereby inhibit peristalsis. May stimulate secretion

A

Enkephalin and related opioid peptides

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22
Q

Present in secretomotor neurons; may play a role in appetite-satiety mechanisms

A

Galanin

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23
Q

May have presynaptic effects on excitatory ENS nerve terminals. Has some relaxant effect on the gut. Prob- ably not a major transmitter in the ENS

A

GABA (γ-aminobutyric acid)

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24
Q

Extremely potent excitatory transmitter to gastrin cells. Also known as mammalian bombesin

A

Gastrin-releasing peptide (GRP)

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25
Q

Found in many noradrenergic neurons. Present in some secretomotor neurons in the ENS and may inhibit secretion of water and electrolytes by the gut.

A

Neuropeptide Y (NPY)

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26
Q

Causes long-lasting vasoconstriction. It is also a cotransmitter in some parasympathetic postganglionic neurons

A

Neuropeptide Y (NPY)

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27
Q

A cotransmitter at inhibitory ENS and other neuromuscular junctions; may be especially important at sphinc- ters

A

Nitric oxide (NO)

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28
Q

The primary transmitter at most sympathetic postganglionic nerve endings

A

Norepinephrine (NE)

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29
Q

An important transmitter or cotransmitter at excitatory neuron-to-neuron junctions in the ENS

A

Serotonin (5-HT)

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30
Q

an important sensory neurotransmitter in the ENS and elsewhere. Tachykinins appear to be excitatory cotransmitters with ACh at ENS neuromuscular junctions. Found with CGRP in cardiovascular sen- sory neurons.

A

Substance P, related tachykinins

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31
Q

Excitatory secretomotor transmitter in the ENS; may also be an inhibitory ENS neuromuscular cotransmitter. A probable cotransmitter in many cholinergic neurons. A vasodilator (found in many perivascular neurons) and cardiac stimulant.

A

Vasoactive intestinal peptide (VIP)

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32
Q

A large number of peripheral ANS fibers synthesize and release acetylcholine; they are ___ fibers; that is, they work by releasing acetylcholine

A

cholinergic

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33
Q

Most postganglionic sympathetic fibers release norepinephrine (also known as noradrenaline); they are __

A

noradrenergic/adrenergic

34
Q

primary acetylcholine receptor subtypes

A

muscarinic and nicotinic receptors

35
Q

receptors that respond to catecholamines

A

adrenoceptor

36
Q

receptors (both muscarinic and nicotinic) that respond to acetylcholine

A

cholinoceptor

37
Q

The general class of adrenoceptors can be further subdivided into

A

α-adrenoceptor, β-adrenoceptor, and dopamine-receptor

38
Q

a neurotoxin derived from chili peppers

A

Capsaicin

39
Q

The sensory fibers in the nonadrenergic, noncholinergic sys- tems are probably better termed

A

“sensory-efferent” or “sensory- local effector” fibers

40
Q

when activated by a sensory input, they are capable of releasing transmitter peptides from the sensory ending itself, from local axon branches, and from collaterals that terminate in the autonomic ganglia.

A

sensory fibers in the nonadrenergic, noncholinergic sys- tems

41
Q

___ sensory fibers in the wall of the urinary bladder significantly influence sympathetic inhibitory outflow to that organ

A

parasympathetic

42
Q

the primary controlled variable in cardiovascular function is ____.

A

mean arterial pressure

43
Q

_____ is transported into the presynaptic nerve terminal by a sodium-dependent choline transporter (CHT)

A

Choline

44
Q

sodium-dependent choline transporter (CHT) can be inhibited by ___ drugs

A

hemicholinium

45
Q

In the cytoplasm, acetylcholine is synthesized from ___ and ___ by the enzyme choline acetyltransferase (ChAT).

A

choline and acetyl-CoA (AcCoA)

46
Q

Acetylcholine (ACh) is transported into the storage vesicle by a ____, which can be inhibited by ___

A

vesicle-associated transporter (VAT)

vesamicol

47
Q

Release of transmitters occurs when voltage-sensitive calcium channels in the terminal membrane are opened, allowing an influx of ___

A

calcium

48
Q

The resulting increase in intracellular calcium causes ___ and exocytotic expulsion of acetylcholine and cotransmitters into the junctional cleft

A

fusion of vesicles with the surface membrane

49
Q

[The resulting increase in intracellular calcium causes fusion of vesicles with the surface membrane and exocytotic expulsion of acetylcholine and cotransmitters into the junctional cleft]

This step can be blocked by ___

A

botulinum toxin

50
Q

Acetylcholine’s action is terminated by metabolism by the enzyme ___.

A

acetylcholinesterase

51
Q

___ is transported into the noradrenergic nerve ending or varicosity by a sodium-dependent carrier

A

Tyrosine

52
Q

Tyrosine is converted to ___, and transported into
the vesicle by the vesicular monoamine transporter (VMAT), which can be blocked by __ and __

A

dopamine

reserpine and tetrabenazine

53
Q

Dopamine is converted to ___ in the vesicle by dopamine-β-hydroxylase

A

NE

54
Q

Fusion of vesicles with the surface membrane results in expulsion of ___

Release can be blocked by drugs such as ___ and ___

A

norepinephrine, cotransmitters, and dopamine-β-hydroxylase.

guanethidine and bretylium

55
Q

After release, norepinephrine diffuses out of the cleft or is transported into the cytoplasm of the terminal by the ____, which can be blocked by ___ and certain antidepressants, or into postjunctional or perijunctional cells.

A

norepinephrine transporter (NET)

cocaine

56
Q

Increased baroreceptor activity causes the ___ central sympathetic outflow and ___ vagal outflow.

A

decreased
increased

57
Q

Presynaptic receptors that respond to the primary transmitter substance released by the nerve ending are called __

A

autoreceptors

58
Q

Postsynaptic regulation can be considered from two perspectives:

modulation by previous activity at the primary receptor

modulation by other simultaneous events

A
59
Q

An extreme form of upregulation occurs after denervation of some tissues, resulting in ___ of the tissue to activators of that receptor type.

A

denervation supersensitivity

60
Q

Drugs that block action potential propagation are very ___ in their action, since they act on a process that is common to all neurons.

A

nonselective

61
Q

drugs that act on the biochemical processes involved in transmitter synthesis and storage are more ___

A

selective

*since the biochemistry of each transmitter differs, eg, norepinephrine synthesis is very different from acetyl- choline synthesis.

62
Q

Parasympathetic nerve activity and muscarinic cholinomimetics mediate ___ of the circular pupillary constrictor muscle and of the ciliary muscle

A

contraction

63
Q

Contraction of the pupillary constrictor muscle causes ___

A

miosis
*a reduction in pupil size

64
Q

Acetylcholine-receptor stimulants and cholinesterase inhibitors make up a large group of drugs that mimic ___

A

acetylcholine

65
Q

mimicked the effects of parasympathetic nerve discharge

A

muscarine

66
Q

The effects of acetylcholine itself and of other cholinomimetic drugs at autonomic neuroeffector junctions are called ___ and are mediated by __ receptors.

A

parasympathomimetic effects

muscarinic

67
Q

Cholinoceptors are members of either ___ on the basis of their structure and transmembrane signaling mechanisms.

A

G protein-linked (muscarinic) or ion channel (nicotinic) families

68
Q

Muscarinic receptors contain ___ transmembrane domains whose third cytoplasmic loop is coupled to __ that function as transducers

A

seven

G proteins

69
Q

___ cholinomimetic agents bind to and activate mus- carinic or nicotinic receptors

A

Direct-acting

70
Q

___ agents produce their primary effects by inhibiting acetylcholinesterase, which hydrolyzes acetylcholine to choline and acetic acid

A

Indirect-acting

71
Q

direct-acting cholinomimetic drugs can be divided on the basis of chemical structure into

A

esters of choline (including acetyl- choline) and alkaloids (such as muscarine and nicotine).

72
Q

Choline esters are poorly absorbed and poorly distributed into the central nervous system because they are __

A

hydrophilic

73
Q

Nicotine, a liquid, is sufficiently ___ to be absorbed across the skin

A

lipid-soluble

74
Q

are well absorbed from the skin, lung, gut, and conjunctiva—thereby making them dangerous to humans and highly effective as insecticides.

A

organophosphate cholinesterase inhibitors (except for echothiophate)

75
Q

The fatal dose of nicotine is approximately ___mg, or 1 drop of the pure liquid.

A

40 mg

76
Q

M1 receptor subtype is located on

A

central nervous system (CNS) neurons

autonomic postganglionic cell bodies

presynaptic sites

77
Q

M2 receptors are located in the

A

myocardium
smooth muscle organs
some neuronal sites

78
Q

M3 receptors are most common on ___

A

effector cell membranes
*especially glandular and smooth muscle cells

79
Q

Muscarinic antagonists are sometimes called ___ because they block the effects of parasympathetic autonomic discharge.

A

parasympatholytic

80
Q

Atropine causes reversible blockade of ___ actions at muscarinic receptors

A

cholinomimetic

PHARMACO PRELIMS (5 decks)

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